82950-64-9Relevant academic research and scientific papers
Voriconazole derivative, synthesis thereof, and use thereof in long-acting preparation
-
, (2017/03/17)
The invention relates to a compound of formula (I), and a salt, an N-oxide, a quaternary ammonium and a stereoisomer thereof. R to R in the formula (I) are as defined in claims. The invention also relates to an intermediate for preparing the compound of formula (I), and a method for preparing the compound of formula (I). The invention further relates to a use of the compound of formula (I) as a drug especially used for preventing or treating fungal infection.
Fosaprepitant derivative, synthesis thereof, and use thereof in long acting preparation
-
, (2017/04/03)
The invention relates to a Fosaprepitant derivative, a synthesis thereof, and a use thereof in a long acting preparation. The invention relates to a compound of formula (I), and a salt, an N-oxide, a quaternary ammonium and a stereoisomer thereof. R to R in the formula (I) are as defined in claims. The invention also relates to an intermediate for preparing the compound of formula (I), and a method for preparing the compound of formula (I). The invention further relates to a use of the compound of formula (I) as a drug especially used for preventing chemotherapy induced acute and late nausea and vomiting.
Posaconazole derivative, synthesis and application in prolonged action preparation thereof
-
, (2017/04/03)
The invention relates to a posaconazole derivative, synthesis and an application in a prolonged action thereof. The invention relates to a formula of a compound and salt, N-oxide, quaternary ammonium and stereoisomer of the compound, wherein R1-R8 are defined according to what is claimed. The invention also relates to a preparation formula of an intermediate body and a method of the compound. The invention further relates to a formula of an application of the compound as a drug, especially the application in preventing or treating fungal infection. The detailed formulas are in the specification.
Method for microwave synthesis of glyceryl caprylate-caprate
-
Paragraph 0029-0032; 0034-0037; 0039-0041; 0043-0046; 0048, (2017/07/20)
The invention provides a preparation method for microwave synthesis of glyceryl caprylate-caprate. Caprylate-caprate and glycerin are reacted in the presence of a compound catalyst, and a glyceryl caprylate-caprate product is prepared by microwave synthesis. According to the method, the molar ratio of caprylate and caprate in the glyceryl caprylate-caprate is regulated, catalysis of the compound catalyst is combined, and a frequency band of 300 to 3,000MHz is adopted for microwave synthesis, so that the high-quality glyceryl caprylate-caprate of which the molar ratio of the caprylate and the caprate is controllable can be efficiently and rapidly prepared. According to the method, a high esterification rate can be achieved, and meanwhile, the energy consumption and the production cost of a reaction process can be remarkably reduced.
Enzymatic synthesis of 1,3-dicaproyglycerol by esterification of glycerol with capric acid in an organic solvent system
Sanchez, Daniel Alberto,Tonetto, Gabriela Marta,Ferreira, Maria Lujan
, p. 7 - 18 (2014/01/06)
In this work, the esterification of glycerol with capric acid catalyzed by an immobilized form of a 1,3-positionally selective lipase (Rhizomucor miehei) showed to be effective for the synthesis of 1,3-dicaprin in n-heptane as the reaction medium. The effects of the reaction parameters were studied using an experimental factorial design of three factors and three levels with two central points. The selected experimental variables were amount of glycerol adsorbed on silica gel (G), biocatalyst load (E) and reaction temperature (T), and the response variables were total conversion of capric acid, acylglycerol fractions, selectivity and yield of dicaprin, and acyl migration reaction. The range of each parameter was selected as follows: G = 50-250 mg, E = 20-40 mg and T = 40-60 C. At optimum conditions 73% capric acid conversion was achieved, with 76% dicaprin selectivity, and selectivity to the specific 1,3-dicaprin of 70% of total products. An adequate selection of the reaction conditions is necessary not only to maximize the conversion of capric acid, but also to minimize the acyl migration reaction and the generation of undesired products. Evidence of kinetically controlled enzymatic acyl migration from sn-3/sn-1 to sn-2 is presented.
New propanoyloxy derivatives of 5β-cholan-24-oic acid as drug absorption modifiers
Coufalová, Lenka,Mrózek, Lech,Rárová, Lucie,Pla?ek, Luká?,Opat?ilová, Radka,Dohnal, Ji?í,Král'Ová, Katarína,Paleta, Old?ich,Král, Vladimír,Dra?ar, Pavel,Jampílek, Josef
, p. 435 - 453 (2013/06/27)
A series of final twelve propanoyloxy derivatives of 5β-cholan-24-oic acid (O-propanoyl derivatives of cholic acid) as potential drug absorption modifiers (skin penetration enhancers, intestinal absorption promoters) was generated by multistep synthesis. Structure confirmation of all generated compounds was accomplished by 1H NMR, 13C NMR, IR and MS spectroscopy methods. All the prepared compounds were analyzed using RP-TLC, and their lipophilicity (RM) was determined. The hydrophobicity (log P), solubility (log S), polar surface area (PSA) and molar volume (MV) of the studied compounds were also calculated. All the target compounds were tested for their in vitro transdermal penetration effect and as potential intestinal absorption enhancers. The cytotoxicity of all the evaluated compounds was evaluated against normal human skin fibroblast cells. Their anti-proliferative activity was also assessed against human cancer cell lines: T-lymphoblastic leukemia cell line and breast adenocarcinoma cell line. One compound showed selective cytotoxicity against human skin fibroblast cells and another compound possessed the highest cytotoxicity against all the tested cell lines. Only one compound expressed anti-proliferative effect on leukemia cancer cells without affecting the growth of normal cells, which should be promising in potential development of new drugs. Most of the target compounds showed minimal anti-proliferative activity (IC50 > 37 μM), indicating they would have moderate cytotoxicity when administered as chemical absorption modifiers. The relationships between the lipophilicity/polarity and the chemical structure of the studied compounds as well as the relationships between their chemical structure and enhancement effect are discussed in this article.
1-O-Alkyl (di)glycerol ethers synthesis from methyl esters and triglycerides by two pathways: Catalytic reductive alkylation and transesterification/reduction
Sutter, Marc,Dayoub, Wissam,Metay, Estelle,Raoul, Yann,Lemaire, Marc
supporting information, p. 786 - 797 (2013/04/24)
From available and bio-sourced methyl esters, monoglycerides or oleic sunflower refined oil, the corresponding 1-O-alkyl (di)glycerol ethers were obtained in both high yields and selectivity by two different pathways. With methyl esters, a reductive alkylation with (di)glycerol was realized under 50 bar hydrogen pressure in the presence of 1 mol% of Pd/C and an acid co-catalyst. A second two step procedure was evaluated from methyl esters or triolein and consisted of a first transesterification to the corresponding monoglyceride with a BaO/Al2O3 catalyst, then its reduction to the desired glycerol monoether with a recyclable heterogeneous catalytic system Pd/C and Amberlyst 35 under H2 pressure. In addition, a mechanism for the reaction was also proposed.
Diaryldiazepine Prodrugs for the Treatment of Neurological and Psychological Disorders
-
Page/Page column 70, (2011/07/29)
The present invention provides prodrug compounds of diaryldiazepine drug compounds.
FOSFLUCONAZOLE DERIVATIVES, SYNTHESIS, AND USE IN LONG ACTING FORMULATIONS
-
Page/Page column 28-30, (2010/10/03)
The invention relates to a compound of formula (I) and the salts, N-oxides, quaternary amines, and stereoisomers thereof, wherein R1 to R8 are as defined in the claims. The invention further relates to intermediates and methods for the preparation of the compounds of formula (I). The invention also relates to the compounds of formula (I) for use as a medicament, particularly for the prevention or treatment of fungal infections.
Conjugated polyelectrolyte based real-time fluorescence assay for phospholipase C
Liu, Yan,Ogawa, Katsu,Schanze, Kirk S.
, p. 150 - 158 (2008/09/17)
A fluorescence turnoff assay for phospholipase C (PLC) from Clostridium perfringens is developed based on the reversible interaction between the natural substrate, phosphatidylcholine, and a fluorescent, water-soluble conjugated polyelectrolyte (CPE). The fluorescence intensity of the CPE in water is increased substantially by the addition of the phospholipid due to the formation of a CPE-lipid complex. Incubation of the CPE-lipid complex with the enzyme PLC causes the fluorescence intensity to decrease (turnoff sensor); the response arises due to PLC-catalyzed hydrolysis of the phosphatidylcholine, which effectively disrupts the CPE-lipid complex. The PLC assay operates with phospholipid substrate concentrations in the micromolar range, and the analytical detection limit for PLC is 2+ and inhibition by EDTA and fluoride ion are demonstrated using the optimized sensor.
